Alkylating Antineoplastic Agents
Antineoplastics
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Alkylating Antineoplastic Agents
Alkylating antineoplastic agents are cytotoxic APIs that form covalent bonds with DNA, leading to cross-linking, strand breaks, and inhibition of replication and transcription. This class includes nitrogen mustards, nitrosoureas, alkyl sulfonates, triazenes, and platinum-based drugs. They are effective against a wide range of hematologic malignancies and solid tumors such as breast cancer, ovarian cancer, sarcomas, and brain tumors. Their mechanism is cell cycle–nonspecific, making them particularly active against rapidly dividing cells. However, their strong cytotoxicity can result in bone marrow suppression, infertility, and secondary malignancies. Despite these risks, alkylating agents remain foundational drugs in many chemotherapeutic regimens due to their broad antitumor activity.
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